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Lofexidine information


Lofexidine
Clinical data
Trade namesBritlofex, Lucemyra, Kai Er Ding, others
AHFS/Drugs.comMonograph
Routes of
administration
By mouth (tablets)
ATC code
  • N07BC04 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability>90%
Protein binding80–90%
MetabolismLiver (glucuronidation)
Elimination half-life11 hours
ExcretionKidney
Identifiers
IUPAC name
  • (RS)-2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
CAS Number
  • 31036-80-3 checkY
PubChem CID
  • 30668
DrugBank
  • DB04948 ☒N
ChemSpider
  • 28460 checkY
UNII
  • UI82K0T627
KEGG
  • D08141 checkY
ChEBI
  • CHEBI:51368 ☒N
ChEMBL
  • ChEMBL17860 checkY
CompTox Dashboard (EPA)
  • DTXSID7023221 Edit this at Wikidata
Chemical and physical data
FormulaC11H12Cl2N2O
Molar mass259.13 g·mol−1
3D model (JSmol)
  • Interactive image
ChiralityRacemic mixture
SMILES
  • Clc2c(OC(C/1=N/CCN\1)C)c(Cl)ccc2
InChI
  • InChI=1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15) checkY
  • Key:KSMAGQUYOIHWFS-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Lofexidine, sold under the brand name Lucemyra among others,[1] is a medication historically used to treat high blood pressure; today, it is more commonly used to help with the physical symptoms of opioid withdrawal.[2] It is taken by mouth.[3] It is an α2A adrenergic receptor agonist.[3] It was approved for use by the Food and Drug Administration in the United States in 2018.[3]

The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[4]

  1. ^ Cite error: The named reference FDA Approval was invoked but never defined (see the help page).
  2. ^ Cite error: The named reference BNF was invoked but never defined (see the help page).
  3. ^ a b c "FDA approves the first non-opioid treatment for management of opioid withdrawal symptoms in adults". U.S. Food and Drug Administration (FDA) (Press release). Retrieved 18 May 2018.
  4. ^ New Drug Therapy Approvals 2018 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2019. Retrieved 16 September 2020.

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Lofexidine

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Lofexidine, sold under the brand name Lucemyra among others, is a medication historically used to treat high blood pressure; today, it is more commonly...

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Opioid withdrawal

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therapy, and symptoms may be relieved by the use of medications including lofexidine and clonidine. Withdrawal from any opioid produces similar signs and symptoms...

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Propofol

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Quetiapine

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Guanfacine Guanoxabenz L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Ibopamine Lofexidine Medetomidine Melevodopa Methyldopa Mivazerol Moxonidine Naphazoline Norepinephrine...

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Propranolol

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Cannabis

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Dimenhydrinate

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ATC code N07

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N07BC01 Buprenorphine N07BC02 Methadone N07BC03 Levacetylmethadol N07BC04 Lofexidine N07BC05 Levomethadone N07BC06 Diamorphine N07BC51 Buprenorphine, combinations...

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Olanzapine

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Prochlorperazine

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Cannabis use disorder

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Combination therapy with dronabinol and the α2-adrenergic receptor agonist lofexidine have shown mixed results, with possible benefits towards reducing withdrawal...

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Flunitrazepam

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Xylazine

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Chloral hydrate

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Ethchlorvynol

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Clozapine

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Phenobarbital

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Chlorpromazine

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Psychiatry

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Hypnotic

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Clenbuterol

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Word Count : 1891

Risperidone

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Guanfacine Guanoxabenz L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Ibopamine Lofexidine Medetomidine Melevodopa Methyldopa Mivazerol Moxonidine Naphazoline Norepinephrine...

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Temazepam

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LSD

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Ramelteon

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Phenothiazine

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